波生坦是一种有效的内皮素-1（ET-1）拮抗剂，在人的平滑肌细胞（SMC）中，它对ETA和ETB受体表现出高亲和力，其Ki值分别为4.7 nM和95 nM。
|
英文别名 (English Synonym) |
Bosentan |
|
中文名称 (Chinese Name) |
波生坦 |
|
靶点 (Target) |
Endothelin Receptor |
|
通路 (Pathway) |
GPCR/G protein |
|
CAS号 (CAS NO.) |
147536-97-8 |
|
分子式 (Formula) |
C27H29N5O6S |
|
分子量 (Molecular Weight) |
551.63 |
|
纯度 (Purity) |
≥98% |
|
溶解性 (Solubility) |
溶于DMSO |
-25~-15℃保存，有效期3年
[1] Dhillon S, Keating GM. Bosentan: a review of its use in the management of mildly symptomatic pulmonary arterial hypertension. Am J Cardiovasc Drugs. 2009;9(5):331-50. doi: 10.2165/11202270-000000000-00000. PMID: 19791841.[2]Iglarz M, Bossu A, Wanner D, Bortolamiol C, Rey M, Hess P, Clozel M. Comparison of pharmacological activity of macitentan and bosentan in preclinical models of systemic and pulmonary hypertension. Life Sci. 2014 Nov 24;118(2):333-9. doi: 10.1016/j.lfs.2014.02.018. Epub 2014 Feb 26. PMID: 24582812.
